Topical/Transdermal Exam 3 Flashcards

1
Q

What are the layers of the skin?

A

-stratum corneum (most superficial)
-living epidermis
-dermis
-hair follicles and sweat glands

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2
Q

Characteristics of stratum corneum

A

-main barrier to permeation
-“brick and mortar” model
-cells are not permeable
-lipid bilayer
-state of hydration is linked to permeability

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3
Q

Characteristics of living epidermis

A

-does not have capillaries
-get their nutrition from the dermis

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4
Q

Characteristics of the dermis

A

-contains capillaries
-must reach this layer to reach systemic action/produce scarring
-has pain, thermal and tactile sensors

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5
Q

Characteristics of hair follicles and sweat glands

A

-secondary route of drug absorption that bypasses the stratum corneum

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6
Q

What are the functions of the skin

A

-containment
-microbial barrier
-chemical barrier
-radiation barrier
-electrical barrier
-thermal barrier and body temperature regulation

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7
Q

Rationale for topical drug delivery

A

good for surface/localized effects

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8
Q

Rationale for transdermal drug delivery

A

Help with reaching some systemic delivery without having to go through the GI tract (degrades faster in the GI tract)

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9
Q

Platforms of topical systems

A

-ointments
-pastes
-creams
-gels
-rigid foams

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10
Q

Different types of ointments

A

-hydrocarbon base
-silicon bases
-absorption bases
-water soluble bases

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11
Q

Examples of hydrocarbon based ointments

A

petrolatum and polyethylene dissolved in mineral oil

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12
Q

Examples of silicone based ointments

A

contains polydimethylsiloxane oil

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13
Q

Examples of absorption based ointments

A

contains W/O emulsifiers

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14
Q

Examples of water soluble bases based ointments

A

polyethylene glycol ointment (due to it’s good H-bonding)

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15
Q

Characteristics of pastes

A

ointments where high concentration of insoluble particulate solids are added

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16
Q

Characteristics of creams

A

O/W or W/O emulsions

17
Q

Characteristics of gel topical systems

A

liquid phase trapped in a matrix of a natural or synthetic polymer

18
Q

Examples of hydrogel topical systems

A

Tragacanth, pectin, carrageenan, methylcellulose, carboxymethylcellulose, carbopol

19
Q

Characteristics of rigid foams

A

air or gas emulsified in a liquid phase (which may contain the drug)

20
Q

What makes a drug suitable for transdermal delivery

A

-short systemic half life, undergoes first-pass metabolism
-high logK value
-<1000 Da in MW

21
Q

Factors affecting drug permeability

A

-hydration
-solubility of drug in the stratum corneum
-excipients (solvents, surfactants)
-pH

22
Q

How does hydration increase drug permeability

A

increased hydration loosens the lipid packing and makes the bilayer more fluid

23
Q

Methods to improve transdermal drug delivery

A

-penetration enhancement
-microneedles

24
Q

Iontophoresis

A

uses LOW voltage electrical current to drive charged drugs through the skin

25
Q

Electroporation

A

uses HIGH, SHORT to create transient pores in the skin

26
Q

Ultrasound

A

uses low frequency ultrasonic energy to disrupt the stratum corneum (sonic waves)

27
Q

Prodrugs

A

modifies the drug structure to make lipophilic

28
Q

Chemical Penetration enhancers

A

dissolves certain parts of the skin to increase permeability

29
Q

Examples of chemical penetration enhancers

A

alcohol, DMSO, surfactants, acetone, ethyl acetate

30
Q

Considerations when using chemical penetration enhancers

A

must rotate sites because if applied it can increase skin wear down and influence dose release rate

31
Q

Dissolving microneedles

A

-drug polymer matrix
-degrades into the skin

32
Q

Hydrogel forming microneedles

A

-has cross linked hydrogel structure
-swells with water and then releases the drug

33
Q

Separable microneedles

A

-drugs are in the tips of the needles
-tips degrade and release the drug

34
Q

Hollow microneedles

A

-needles are hollow and allow for drug solutions to be injected

35
Q

Potential mistakes patients may make with transdermal patches

A

-preparation
-removal
-application
-monitoring
-storage and disposal

36
Q

What do patients not realize when using transdermal patches

A

-patch must be applied directly to the skin
-must remove protective liner
-use one patch at a time
-where to place (rotate the area)

37
Q

Drugs in transdermal patches

A

-nicotine
-clonidine
-nitroglycerin
-estradiol
-scoplamine
-fentanyl
-rivastigmine